EC50 values of methamphetamine and amphetamine for hOCT1 and hOCT2 determined by two-binding site fitting
The EC50 values were obtained by fitting inhibition data in Fig. 1 and Supplemental Fig. 2 using eq. 2 described in Materials and Methods with the fit shown in Supplemental Fig. 3. The last column lists the P values obtained by comparing eqs. 1 and 2 with an extra sum-of-squares F test. Results represent mean ± S.D. of three independent experiments each run in triplicate.
Inhibitor | Two-Binding Site | Two-Binding versus One-Binding Site | ||
---|---|---|---|---|
Transporter | EC50 Value | |||
High Affinity | Low Affinity | |||
μM | μM | |||
Methamphetamine | hOCT1 | 5.29 ± 0.66 | 400 ± 229 | P < 0.0001 |
hOCT2 | 1.21 ± 0.19 | 58.2 ± 23.4 | P < 0.0001 | |
Amphetamine | hOCT1 | NA | NA | P = 0.55 |
hOCT2 | 0.72 ± 0.29 | 145 ± 104 | P < 0.0001 |
NA, not applicable.